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Effects of cannabidiol on the function of α7-nicotinic acetylcholine receptors.
Eur J Pharmacol. 2013 Nov 15; 720(1-3):310-9.EJ

Abstract

The effects of cannabidiol (CBD), a non-psychoactive ingredient of cannabis plant, on the function of the cloned α7 subunit of the human nicotinic acetylcholine (α7 nACh) receptor expressed in Xenopus oocytes were tested using the two-electrode voltage-clamp technique. CBD reversibly inhibited ACh (100 μM)-induced currents with an IC50 value of 11.3 µM. Other phytocannabinoids such as cannabinol and Δ(9)-tetrahydrocannabinol did not affect ACh-induced currents. CBD inhibition was not altered by pertussis toxin treatment. In addition, CBD did not change GTP-γ-S binding to the membranes of oocytes injected with α7 nACh receptor cRNA. The effect of CBD was not dependent on the membrane potential. CBD (10 µM) did not affect the activity of endogenous Ca(2+)-dependent Cl(-) channels, since the extent of inhibition by CBD was unaltered by intracellular injection of the Ca(2+) chelator BAPTA and perfusion with Ca(2+)-free bathing solution containing 2mM Ba(2+). Inhibition by CBD was not reversed by increasing ACh concentrations. Furthermore, specific binding of [(125)I] α-bungarotoxin was not inhibited by CBD (10 µM) in oocytes membranes. Using whole cell patch clamp technique in CA1 stratum radiatum interneurons of rat hippocampal slices, currents induced by choline, a selective-agonist of α7-receptor induced currents were also recoded. Bath application of CBD (10 µM) for 10 min caused a significant inhibition of choline induced currents. Finally, in hippocampal slices, [(3)H] norepinephrine release evoked by nicotine (30 µM) was also inhibited by 10 µM CBD. Our results indicate that CBD inhibits the function of the α7-nACh receptor.

Authors+Show Affiliations

Laboratory of Functional Lipidomics, Department of Pharmacology, College of Medicine and Health Sciences, UAE University, Abu Dhabi, Al Ain, United Arab Emirates.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

24140434

Citation

Mahgoub, Mohamed, et al. "Effects of Cannabidiol On the Function of Α7-nicotinic Acetylcholine Receptors." European Journal of Pharmacology, vol. 720, no. 1-3, 2013, pp. 310-9.
Mahgoub M, Keun-Hang SY, Sydorenko V, et al. Effects of cannabidiol on the function of α7-nicotinic acetylcholine receptors. Eur J Pharmacol. 2013;720(1-3):310-9.
Mahgoub, M., Keun-Hang, S. Y., Sydorenko, V., Ashoor, A., Kabbani, N., Al Kury, L., Sadek, B., Howarth, C. F., Isaev, D., Galadari, S., & Oz, M. (2013). Effects of cannabidiol on the function of α7-nicotinic acetylcholine receptors. European Journal of Pharmacology, 720(1-3), 310-9. https://doi.org/10.1016/j.ejphar.2013.10.011
Mahgoub M, et al. Effects of Cannabidiol On the Function of Α7-nicotinic Acetylcholine Receptors. Eur J Pharmacol. 2013 Nov 15;720(1-3):310-9. PubMed PMID: 24140434.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of cannabidiol on the function of α7-nicotinic acetylcholine receptors. AU - Mahgoub,Mohamed, AU - Keun-Hang,Susan Yang, AU - Sydorenko,Vadym, AU - Ashoor,Abrar, AU - Kabbani,Nadine, AU - Al Kury,Lina, AU - Sadek,Bassem, AU - Howarth,Christopher F, AU - Isaev,Dmytro, AU - Galadari,Sehamuddin, AU - Oz,Murat, Y1 - 2013/10/18/ PY - 2013/06/15/received PY - 2013/09/16/revised PY - 2013/10/07/accepted PY - 2013/10/22/entrez PY - 2013/10/22/pubmed PY - 2014/8/16/medline KW - 1,2-bis (o-aminophenoxy) ethane-N, N,N′,N′-tetraacetic acid KW - 4-(2-hydroxyethyl) piperazineethane sulfonic acid KW - ACh KW - ANOVA KW - BAPTA KW - Cannabidiol KW - Cannabinoids KW - DMSO KW - HEPES KW - MBS KW - Nicotinic receptors KW - PTX KW - Xenopus oocyte KW - acetylcholine KW - analysis of variance KW - dimethyl sulfoxide KW - modified Barth's solution KW - pertussis toxin. SP - 310 EP - 9 JF - European journal of pharmacology JO - Eur J Pharmacol VL - 720 IS - 1-3 N2 - The effects of cannabidiol (CBD), a non-psychoactive ingredient of cannabis plant, on the function of the cloned α7 subunit of the human nicotinic acetylcholine (α7 nACh) receptor expressed in Xenopus oocytes were tested using the two-electrode voltage-clamp technique. CBD reversibly inhibited ACh (100 μM)-induced currents with an IC50 value of 11.3 µM. Other phytocannabinoids such as cannabinol and Δ(9)-tetrahydrocannabinol did not affect ACh-induced currents. CBD inhibition was not altered by pertussis toxin treatment. In addition, CBD did not change GTP-γ-S binding to the membranes of oocytes injected with α7 nACh receptor cRNA. The effect of CBD was not dependent on the membrane potential. CBD (10 µM) did not affect the activity of endogenous Ca(2+)-dependent Cl(-) channels, since the extent of inhibition by CBD was unaltered by intracellular injection of the Ca(2+) chelator BAPTA and perfusion with Ca(2+)-free bathing solution containing 2mM Ba(2+). Inhibition by CBD was not reversed by increasing ACh concentrations. Furthermore, specific binding of [(125)I] α-bungarotoxin was not inhibited by CBD (10 µM) in oocytes membranes. Using whole cell patch clamp technique in CA1 stratum radiatum interneurons of rat hippocampal slices, currents induced by choline, a selective-agonist of α7-receptor induced currents were also recoded. Bath application of CBD (10 µM) for 10 min caused a significant inhibition of choline induced currents. Finally, in hippocampal slices, [(3)H] norepinephrine release evoked by nicotine (30 µM) was also inhibited by 10 µM CBD. Our results indicate that CBD inhibits the function of the α7-nACh receptor. SN - 1879-0712 UR - https://www.unboundmedicine.com/medline/citation/24140434/Effects_of_cannabidiol_on_the_function_of_α7_nicotinic_acetylcholine_receptors_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0014-2999(13)00754-1 DB - PRIME DP - Unbound Medicine ER -